title: Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR α/γ activators.
abstract: In our search for new PPARα/γ agonists, we designed and synthesized a series of benzoylazole-based carboxylic acids. Compound 9 showed potent PPARγ partial agonistic activity with modest PPARα agonistic activity. The sodium salt of 9 (9Na) demonstrated potent efficacy in lowering both blood glucose and lipids in an animal model without causing significant body weight gain, a well-known side effect associated with PPARγ full agonists.
authors.affiliation: Dainippon Sumitomo Pharma Co, Ltd, Drug Research Division, Chemistry Research Laboratories, Osaka, Japan. kantaro-ushiroda@ds-pharma.co.jp
authors.forename: Kantaro
authors.initials: K
authors.lastname: Ushiroda
authors.forename: Katsunori
authors.initials: K
authors.lastname: Maruta
authors.forename: Takeshi
authors.initials: T
authors.lastname: Takazawa
authors.forename: Tomokazu
authors.initials: T
authors.lastname: Nagano
authors.forename: Mutsuo
authors.initials: M
authors.lastname: Taiji
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Kohno
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Sato
authors.forename: Shinji
authors.initials: S
authors.lastname: Horai
authors.forename: Kazunori
authors.initials: K
authors.lastname: Yanagi
authors.forename: Ryu
authors.initials: R
authors.lastname: Nagata
mesh_terms: D000818:Animals; D001393:Azoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D023421:Models, Animal; D008958:Models, Molecular; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*
chemical_list: D001393:Azoles; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D047493:PPAR alpha; D047495:PPAR gamma